신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1H-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물
    41.
    发明公开
    신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1H-피라졸 화합물,이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-(3,4-二甲氧基苯基) - 乙基] -1H-吡唑化合物,其制备方法和包含其的药物组合物

    公开(公告)号:KR1020080065722A

    公开(公告)日:2008-07-15

    申请号:KR1020070002715

    申请日:2007-01-10

    Abstract: A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.

    Abstract translation: 提供了一种新型化合物,以显示对PDE-4酶的优异活性和对其他PDE酶的高选择性,从而被用作炎症相关疾病,关节炎,特应性皮炎,白血病,各种癌症和退行性脑病的治疗剂 效果。 1-(1-(3,4-二烷氧基苯基) - 烷基] -1H-吡唑化合物由式(1)表示,通过式(2)表示的卤代苄基化合物与吡唑化合物 由公式(3)表示。 在式(1)中,每个R 1和R 2独立地为H,可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基,C 3-7环烷基,(C 3-7)环烷基(C 1-7) 烷基,芳基或杂芳基,芳(C 1-5)烷基或芳(C 1-5)烷氧基,或者R 1和R 2可以被C 1-3亚烷基相互连接; 每个R 3,R 4和R 5独立地为H,苯基,吡啶基,N-氧代吡啶基,直链或支链饱和和不饱和C 1-7烷基,C 3-7环烷基,(C 3-10)环烷基(C 1-7)烷基,卤素,氰基 ,硝基,氨基,单或二(C1-7)烷基氨基,单或二(C1-7)烷基氨基羰基,C3-7环烷基氨基,3至7元饱和或不饱和杂环,包括O,N或S,胍基 (C 1-7)烷基,羟基(C 1-7)烷基,羧基或(C 1-7)烷氧基羰基;(C 1-7)烷氧基, R6是直链或支链饱和和不饱和的C1-7烷基,C3-7环烷基,(C3-10)环烷基(C1-7)烷基,苯基,苯氧基,苄基,苄氧基,C1-7烷氧基或(C1-7) 烷氧基(C 1-7)烷基。 用于治疗或预防与气道炎症,关节炎,特应性皮炎,白血病,癌症或退行性脑疾病相关的疾病的药物组合物包括1- [1-(3,4-二烷氧基苯基) - 烷基] -1H-吡唑衍生物作为有效的 成分。

    7-(3,4-디알콕시페닐)-피라졸로[1,5-a]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물
    42.
    发明授权
    7-(3,4-디알콕시페닐)-피라졸로[1,5-a]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물 失效
    7-(3,4-디알콕시페닐) - 피라졸로[1,5-α]피리미딘화합물을포함하는관절염,아토피피부염,백혈병을포함한암및알쯔하이머,우울증또는기억력감소등의뇌질환의치료및 예방을위약제제학적조성

    公开(公告)号:KR100753017B1

    公开(公告)日:2007-08-30

    申请号:KR1020060046860

    申请日:2006-05-25

    Abstract: A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.

    Abstract translation: 用于治疗或预防关节炎,特应性皮炎,肿瘤和退行性脑疾病,其包括7-(3,4-二烷氧基) - 吡唑并提供[1,5-a]嘧啶化合物抑制PDE-4的活性(phosphodiesterase-的药物组合物 4)并通过减少HARBS(高亲和力咯利普兰结合位点)亲和力来减少副作用,例如呕吐。 用于治疗或预防关节炎,特应性皮炎,肿瘤和退行性脑疾病的药物组合物包含7-(3,4-二烷氧基) - 吡唑并[1,5-a]嘧啶化合物由式(1)表示,其中R1和R2 (C 1 -C 7)烷基,含有卤素原子的直链或支链饱和或不饱和(C 1 -C 7)烷基,(C 3 -C 7)环烷基,含有3至7元杂环烷基的3元至7元杂环烷基 (C4-C10)环烷基(C1-C7)烷基,在杂环中含有氧,氮或硫的3元至7元杂环烷基(C1-C7)烷基,苯基 ,苄基或烯丙基; (C 1 -C 7)烷基,(C 1 -C 7)烷氧基,(C 1 -C 7)烷氧基(C 1 -C 7)烷基,(C 1 -C 7)烷氧基, (C 1 -C 7)烷基,羧酸,羧基(C 1 -C 7)烷基酯,羧基(C 1 -C 7)烷基酰胺,氨基或单或二(C 1 -C 7)烷基氨基羰基; (C 1 -C 7)烷基,(C 3 -C 7)环烷基,(C 1 -C 7)烷氧基,(C 1 -C 7)烷氧基(C 1 -C 7)烷基,羟基(C 1 -C 7)烷基, C1-C7)烷基酮,(C1-C10)烷基羧酸,羧基(C1-C10)烷基酯,羧基(C1-C10)烷基酰胺,氨基,单或二(C1-C7)烷基氨基,单或二(C1-C7 )烷基氨基羰基,(C3-C7)环烷基胺,吗啉,氧化吗啉,哌啶,哌嗪,哌嗪氧化物或芳基。

    제초활성을 갖는9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체
    44.
    发明公开
    제초활성을 갖는9-(5-이속사졸메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체 失效
    9-(5-异丙氧基苯基)亚氨基-8-三氮杂-1,6-二氮杂双环(4.3.0)含有除草活性的非 - 7-酮衍生物和含有其的除草剂组合物作为活性成分

    公开(公告)号:KR1020040092186A

    公开(公告)日:2004-11-03

    申请号:KR1020030026416

    申请日:2003-04-25

    Abstract: PURPOSE: Provided are 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivatives which have herbicidal activity and a herbicidal composition containing the same as active ingredient. The derivatives have high stability to rice and excellent herbicidal effect. CONSTITUTION: 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivative is represented by the formula(1), wherein R is C1-C5 alkyl group, phenyl group or substituted phenyl group in which the substituted phenyl group has a substituent selected from C1-C3 alkoxy group, halogen atom, cyano group and carboxylic acid ester group. The herbicidal composition is characterized by containing the 9-(5-isoxazolemethoxyphenyl)imino-8-thia-1,6-diazabicyclo(4.3.0)nonan-7-one derivative as active ingredient.

    Abstract translation: 目的:提供具有除草活性的9-(5-异恶唑甲氧基苯基)亚氨基-8-硫杂-1,6-二氮杂双环(4.3.0)壬-7-酮衍生物和含有与活性成分相同的除草组合物。 该衍生物对水稻的稳定性高,除草效果好。 构型:9-(5-异恶唑甲氧基苯基)亚氨基-8-硫杂-1,6-二氮杂双环(4.3.0)壬-7-酮衍生物由式(1)表示,其中R是C1-C5烷基,苯基 基团或取代的苯基,其中取代的苯基具有选自C 1 -C 3烷氧基,卤素原子,氰基和羧酸酯基的取代基。 除草组合物的特征在于含有9-(5-异恶唑甲氧基苯基)亚氨基-8-硫杂-1,6-二氮杂双环(4.3.0)壬-7-酮衍生物作为活性成分。

    제초활성을 갖는2-(5-옥시란일메톡시페닐)-4,5,6,7-테트라히드로-2H-인다졸유도체
    45.
    发明公开
    제초활성을 갖는2-(5-옥시란일메톡시페닐)-4,5,6,7-테트라히드로-2H-인다졸유도체 失效
    杀虫剂2-(5-氧代甲氧基苯基)-4,5,6,7-四氢-2H-吲唑衍生物,用于选择性杀死

    公开(公告)号:KR1020040086696A

    公开(公告)日:2004-10-12

    申请号:KR1020030021052

    申请日:2003-04-03

    Abstract: PURPOSE: Herbicidal2-(5-oxiranylmethoxyphenyl)-4,5,6,7-tetrahydro-2H-indazole derivatives are provided, which compounds have improved herbicidal effects and selectivity, so that the compounds can selectively kill weeds. CONSTITUTION: The herbicidal2-(5-oxiranylmethoxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole derivatives represented by formula (1) are provided, wherein R1, R2 and R3 are independently hydrogen, C1-C5 alkyl, phenyl or substituted phenyl with 1 to 3 of halogen atoms. The method for preparing the herbicidal2-(5-oxiranylmethoxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole derivatives of formula (1) comprises the steps of: reacting a compound of formula (2) with allyl halide in the presence of base to prepare a compound of formula (3); and introducing epoxy group into a double bond of the compound of formula (3), wherein X is halogen.

    Abstract translation: 目的:提供除草剂2-(5-环氧乙烷基甲氧基苯基)-4,5,6,7-四氢-2H-吲唑衍生物,该化合物具有改善的除草效果和选择性,使得化合物可以选择性地杀死杂草。 构成:提供由式(1)表示的除草2-(5-环氧乙烷基甲氧基苯基)-4,5,6,7-四氢-2H-吲唑衍生物,其中R 1,R 2和R 3独立地是氢,C 1 -C 5烷基,苯基 或具有1至3个卤素原子的取代的苯基。 制备式(1)的除草-2-(5-环氧乙烷基甲氧基苯基)-4,5,6,7-四氢-2H-吲唑衍生物的方法包括以下步骤:使式(2)的化合物与烯丙基卤在 碱的存在以制备式(3)的化合物; 并将环氧基引入到式(3)化合物的双键中,其中X是卤素。

    제초활성을 갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체
    46.
    发明公开
    제초활성을 갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체 失效
    9-(5-异丙氧基乙基苯基)亚氨基-8-三噻基-1,6-二氮杂双环[4.3.0 |具有除草活性的非 - 7-酮衍生物

    公开(公告)号:KR1020040017892A

    公开(公告)日:2004-03-02

    申请号:KR1020020049819

    申请日:2002-08-22

    Abstract: PURPOSE: Provided are derivatives of 9-(5-isoxazolinemethoxyphenyl)imino-8-thia-1.6-diazabicylco£4.3.0|nonane-7-one, represented by the formula(1) and herbicides containing them as active ingredients and having excellent herbicidal activity and selectivity when applied to a rice paddy. CONSTITUTION: Derivatives are represented by the formula(1), wherein R is C1-C6 alkyl, phenyl or substituted phenyl, wherein substituents are 1-3 of halogen atom, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 haloalkyl, cyano, nitro, carboxyl and esters of carboxy acid.

    Abstract translation: 目的:提供由式(1)表示的9-(5-异恶唑啉甲氧基苯基)亚氨基-8-硫杂-1,6-二氮杂双环[4.3.0]壬烷-7-酮和含有它们作为活性成分并具有优异的除草剂的衍生物 施用于水稻时的除草活性和选择性。 构成:衍生物由式(1)表示,其中R是C1-C6烷基,苯基或取代的苯基,其中取代基是1-3的卤素原子,C1-C3烷基,C1-C3烷氧基,C1-C3卤代烷基, 氰基,硝基,羧基和羧酸的酯。

    3-클로로-2-(4-클로로-2-플루오로-5-히드록시페닐)-4,5,6,7-테트라히드로-2H-인다졸의 제조방법
    47.
    发明公开
    3-클로로-2-(4-클로로-2-플루오로-5-히드록시페닐)-4,5,6,7-테트라히드로-2H-인다졸의 제조방법 失效
    制备3-氯-2-(4-氯-2-氟-5-羟基苯基)-4,5,6,7-四氢-2H-吲哚的方法

    公开(公告)号:KR1020030095677A

    公开(公告)日:2003-12-24

    申请号:KR1020020033207

    申请日:2002-06-14

    Abstract: PURPOSE: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole is provided, thereby improving its preparation yield and converting by-products of the preparation into starting material. CONSTITUTION: A process for preparing 3-chloro-2- (4-chloro-2-fluoro-5-hydroxyphenyl)- 4,5,6,7-tetrahydro-2H-indazole of the formula 1 comprises the steps of: reacting 2- (2-fluoro-4-chloro-5-hydroxyphenyl)- 2,3a,4,5,6,7- hexahydroindazole-3-one of the formula 2 with phosgene; concentrating the phosgene reaction mixture under reduced pressure; dissolving the concentrate in an organic solvent; adding ammonia water or hydroxide solution to the organic solvent and filtering solids; and distilling the filtrated solution, wherein the organic solvent is ethylacetate; the addition of ammonia water or hydroxide solution is carried out at room temperature; the solids are mainly constituted of a compound of the formula 2, and the by-products of the reaction include a dimer represented by the formula 3a, 3b or 3c.

    Abstract translation: 目的:提供3-氯-2-(4-氯-2-氟-5-羟基苯基)-4,5,6,7-四氢-2H-吲唑的制备方法,从而提高其制备产率,并通过 - 制备成原料的产品。 构成:式1的3-氯-2-(4-氯-2-氟-5-羟基苯基)-4,5,6,7-四氢-2H-吲唑的制备方法包括以下步骤:使2 - (2-氟-4-氯-5-羟基苯基)-2,3a,4,5,6,7-六氢吲唑-3-酮与光气; 在减压下浓缩光气反应混合物; 将浓缩物溶解在有机溶剂中; 向有机溶剂中加入氨水或氢氧化物溶液并过滤固体; 并蒸馏过滤的溶液,其中有机溶剂是乙酸乙酯; 在室温下加入氨水或氢氧化钠溶液; 固体主要由式2的化合物构成,反应的副产物包括由式3a,3b或3c表示的二聚体。

    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체화합물
    49.
    发明公开
    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체화합물 有权
    具有除草活性的5-苄氧基甲基-1,6-异恶唑烷酮衍生物

    公开(公告)号:KR1020020019750A

    公开(公告)日:2002-03-13

    申请号:KR1020000052917

    申请日:2000-09-07

    CPC classification number: A01N43/80

    Abstract: PURPOSE: Provided is 5-benzyloxymethyl-1,2-isoxazoline derivative which has an excellent herbicidal activity. Also, provided are its manufacturing method and herbicides containing the derivative as an active ingredient. CONSTITUTION: 5-benzyloxymethyl-1,2-isoxazoline derivative is represented by the formula(I), wherein X1, X2 and X3 individually represent hydrogen, methyl group, ethyl group, halogen group, methoxy group or nitro group (provided that it is an exception that X1, X2 and X3 are decimals all together); Y1, Y2 and Y3 are individually hydrogen or fluorine.

    Abstract translation: 目的:提供具有优异除草活性的5-苄氧基甲基-1,2-异恶唑啉衍生物。 此外,其制造方法和含有该衍生物作为活性成分的除草剂。 构成:5-苄氧基甲基-1,2-异恶唑啉衍生物由式(I)表示,其中X1,X2和X3各自表示氢,甲基,乙基,卤素基,甲氧基或硝基(条件是它是 一个例外,X1,X2和X3都是小数) Y1,Y2和Y3分别为氢或氟。

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